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Cat. No.: HY-110328

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PKI-166 hydrochloride

Name: PKI-166 hydrochloride
Brand: MedChemExpress
SKU: HY-110328
Availability: PreOrder

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC₅₀ of 0.7 nM.

For research use only. We do not sell to patients.

CAS No.: 2230253-82-2
Formula: C₂₀H₁₉ClN₄O
Molecular Weight:366.84

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

PKI-166 hydrochloride Chemical Structure

CAS No.: 2230253-82-2

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC₅₀ of 0.7 nM^[1].

IC₅₀ & Target

IC50: 0.7 nM (EGFR tyrosine kinase)^[1]

All EGFR Isoforms :

In Vitro

PKI-166 hydrochloride (0-0.5 μM; 1 hour; pretreatment) inhibits EGFR autophosphorylation in human pancreatic cancer cells^[1].
PKI-166 hydrochloride (0.03 μM; 6 days) enhances the cytotoxicity mediated by gemcitabine^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

Cell Line:

L3.6pl cells
Concentration:

0.01 μM, 0.05 μM, 0.5 μM
Incubation Time:

1 hour
Result:

Inhibited EGFR autophosphorylation in a dose-dependent manner.

Cell Cytotoxicity Assay^[1]

View Protocol

Cell Line:

L3.6pl cells
Concentration:

0.03 μM
Incubation Time:

6 days
Result:

Enhanced the cytotoxicity mediated by gemcitabine.

In Vivo

PKI-166 hydrochloride (100 mg/kg; p.o.; daily; for 29 days) inhibits of pancreatic cancer growth^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male athymic nude mice with L3.6pl cells xenograft (8-12 weeks)^[1]
Dosage:

100 mg/kg
Administration:

Oral administration; daily; for 29 days
Result:

Significantly decreased median tumor volume.

Chemical Information

CAS No. 2230253-82-2
Molecular Weight 366.84
Formula C₂₀H₁₉ClN₄O
SMILES

OC1=CC=C(C2=CC3=C(N=CN=C3N2)N[C@H](C)C4=CC=CC=C4)C=C1.Cl[H]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Bruns CJ, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 2000 Jun 1;60(11):2926-35. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

PKI-166 hydrochloride

1 Cited Publications

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Protocols
Purity & Documentation
References

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PKI-166 hydrochloride

Publications Citing Use of MedChemExpress (MCE) PKI-166 hydrochloride

All EGFR Isoforms